Use this url to cite publication: https://hdl.handle.net/20.500.12512/88641
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Anticancer activity and ADMET properties of resorcinol-bearing lead compounds / Vilma Petrikaitė
Type of publication
Tezės kitame recenzuojamame leidinyje / Theses in other peer-reviewed publication (T1e)
Author(s)
Vilniaus universitetas |
Title
Anticancer activity and ADMET properties of resorcinol-bearing lead compounds / Vilma Petrikaitė
Publisher (trusted)
Baltijos pažangių technologijų institutas - BPTI |
Date Issued
Date Issued |
---|
2011-06-30 |
Extent
p. 17-18.
Is part of
Scientific Camp Smithy of Ideas 2001 : Trakai, Lithuania, June 30-July 3, 2011 : Book of abstracts / Lithuanian Society of Young Researchers ; Edited by: Marija Eidukevičiūtė, Eugenijus Keras, Vilma Petrikaitė. [Vilnius] : Baltic Institute of Advanced Technology, 2011. ISBN 978-9955-875-01-7.
Version
Originalus / Original
Field of Science
Abstract
Heat-shock protein 90 (Hsp90) constitutes about 1-2% of total cellular proteins and is usually present in the cell as a dimer. Hsp90 is a promising anticancer drug target, as cancerous cells are more susceptible to Hsp90 inhibition than normal cells. A large number of different Hsp90 inhibitors have been synthesized to date, but only several of them made to clinical trials. Therefore, there is a great need for new potent Hsp90 inhibitors with improved activity, selectivity, solubility, reduced toxicity and side-effects, as well reduced cost of synthesis. A group of compounds similar to the diarylpyrazole resorcinol class of inhibitors was chemically synthesized. The structure-activity relationship of the compounds was determined in vitro and cell biology methods. Compound binding to Hsp90 was measured by isothermal titration calorimetry (ITC) and the thermal shift assay (TSA). Growth inhibition was determined for two cancer cell lines: cervical cancer (HeLa) and osteosarcoma (U2OS). Main pharmacokinetic and toxicological parameters were estimated in silico by using ADME/Tox Boxes software. Toxicity was determined on mice by method of fixed doses. [...].
Type of document
type::text::conference output::conference proceedings::conference paper
ISBN (of the container)
978-9955-875-01-7
Other Identifier(s)
(LSMU ALMA)990000779630107106
Coverage Spatial
Lietuva / Lithuania (LT)
Language
Anglų / English (en)